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Celastrol

现货
Catalog No.
A2604
抗氧化、抗炎和免疫抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,000.00
现货
5mg
¥ 500.00
现货
25mg
¥ 1,500.00
现货

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Background

Celastrol is a potent proteasome inhibitor [1].Proteasomes are protein complexes that degrading unneeded or damaged proteins by proteolysis.
Celastrol is a potent proteasome inhibitor and an antioxidant, anti-inflammatory and immunosuppressive agent. In a cell-free proteasome activity assay, Celastrol inhibits the chymotrypsin-like activity of a purified rabbit 20S proteasome at 2.5umol and human prostate cancer cellular 26S proteasome at 1-5 μmol. In PC-3 and LNCaP (AR-positive) cells, Celastrol results in the accumulation of ubiquitinated proteins and proteasome substrates (IKB-A, Bax, and p27), and induction of apoptosis [1]. In KBM-5 cells, Celastrol enhances TNF-induced apoptosis by 2% to 92%. In the tumor cells, Celastrol inhibited TNF-induced tumor-cell invasion by 12-fold [2]. In human PBMCs, Celastrol inhibited LPS-induced TNF-α production with IC50 value of 70 nM and LPS-induced IL 113 production with IC50 value of 30nM in a dose-dependent way [3].
In PC-3 tumor–bearing nude mice, Celastrol (1-3 mg/kg/d,1-31 days) inhibited the tumor growth by 65-93% [1].  
References:
[1]. Yang H, Chen D, Cui QC, et al. Celastrol, a triterpene extracted from the Chinese "Thunder of God Vine," is a potent proteasome inhibitor and suppresses human prostate cancer growth in nude mice. Cancer Res, 2006, 66(9): 4758-4765.
[2]. Allison AC, Cacabelos R, Lombardi VR, et al. Celastrol, a potent antioxidant and anti-inflammatory drug, as a possible treatment for Alzheimer's disease. Prog Neuropsychopharmacol Biol Psychiatry, 2001, 25(7):,1341-1357.
[3]. Sethi G, Ahn KS, Pandey MK, et al. Celastrol, a novel triterpene, potentiates TNF-induced apoptosis and suppresses invasion of tumor cells by inhibiting NF-kappaB-regulated gene products and TAK1-mediated NF-kappaB activation. Blood, 2007, 109(7): 2727-2735.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt450.61
Cas No.34157-83-0
FormulaC29H38O4
Solubility≥22.55mg/mL in DMSO
Chemical Name(2R,4aS,6aR,6aS,14aS,14bR)-10-hydroxy-2,4a,6a,6a,9,14a-hexamethyl-11-oxo-1,3,4,5,6,13,14,14b-octahydropicene-2-carboxylic acid
SDFDownload SDF
Canonical SMILESCC1=C(C(=O)C=C2C1=CC=C3C2(CCC4(C3(CCC5(C4CC(CC5)(C)C(=O)O)C)C)C)C)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

激酶实验 [1]:

纯化的20S 蛋白酶体活性抑制实验

将纯化的兔20S蛋白酶体 (0.1 μg) 与40 μM各种荧光多肽底物加入100 μL实验缓冲液 (20 mM Tris-HCl (pH 7.5))中,再加入不同浓度的Celastrol或DMSO,于37℃下,孵育2小时。测定每种蛋白酶体活性的抑制情况。

细胞实验 [1]:

细胞系

雄性激素非依赖性的PC-3前列腺癌细胞

制备方法

在DMSO中的溶解度大于22.6 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

0.5 ~ 5 μM

实验结果

在PC-3细胞中,Celastrol呈浓度依赖性地显著抑制蛋白酶体糜蛋白酶活性。此外,Celastrol呈浓度依赖性地提升泛素化蛋白水平。在经Celastrol处理的PC-3细胞中,IκB-α、Bax和p27水平也有所提升。

动物实验 [1]:

动物模型

携带C4-2B肿瘤的裸小鼠

给药剂量

1或3 mg/kg/day;腹腔注射;持续16天

实验结果

在携带C4-2B肿瘤的裸小鼠中,Celastrol (3 mg/kg) 显著抑制肿瘤生长(高达70%),上述结果与p27和Bax水平升高相关。在3 mg/kg剂量下,Celastrol也促进肿瘤细胞凋亡,同时,异种移植肿瘤中出现各种PARP剪切片段。此外,Celastrol (3 mg/kg) 引起35%的肿瘤抑制,上述结果与蛋白酶体活性降低以及AR蛋白表达下调相关。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Yang H, Chen D, Cui QC, et al. Celastrol, a triterpene extracted from the Chinese "Thunder of God Vine," is a potent proteasome inhibitor and suppresses human prostate cancer growth in nude mice. Cancer Res, 2006, 66(9): 4758-4765.

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